5-(2,8-Bis(trifluoromethyl)quinolin-4-yloxymethyl)isoxazole-3-carboxylic acid ethyl ester (compound 3) was reported to have excellent antituberculosis activity against both replicating and non-replicating Mycobacterium tuberculosis, with a minimum inhibitory concentration (MIC) of 0.9 μM and 12...

SN-38 is the active metabolite of irinotecan, an FDA-approved chemotherapeutic agent indicated for colorectal carcinoma, which would not be clinically applicable due to its very poorly soluble and hydrolytic degradation properties. To overcome these limitations, it was proposed to conjugate SN38...

AimsPiperazinic derivatives have therapeutic potential by acting as analgesic, antidepressant-like, anticonvulsant and antipsychotic in preclinical studies. In order to develop new drugs to treat mental disorders, we designed and synthesized the 4-(1-phenyl-1H-pyrazol-4-ylmethyl)-piperazine-1-ca...

AimsClinical complaints on the first-line of cardiovascular medications make continuous search for new drugs a necessity. This study evaluated the cardiovascular effects and mechanism of 4-[(1-phenyl-1H-pyrazol-4-yl)methyl]1-piperazine carboxylic acid ethyl ester (LQFM008).

N-[(1,5,9)-trimethyldecyl]-4α, 10-dimethyl-8-aza-trans-decal-3β-ol (8-azadecalin 1), a highenergy intermediate analogue for the 2,3-oxidosqualene-lanosterol cyclase, was found to be a powerful (ic50≈ 0.1 μM) inhibitor of cholesterol biosynthesis in human hepatoma HepG2 cells. In analogy with...

10-Aza-10,11-dihydro-2,3-oxidosqualene (10 N-OS), 19-aza-18,19,22,23-tetrahydro-2,3-oxidosqualene (19 N-OS) and 23-aza-22,23-dihydro-2,3-oxidosqualene (23 N-OS), designed as analogues of carbocationic intermediates involved in the reaction pathway of 2,3-oxidosqualene-cycloartenol cyclase (OSCC)...

The inhibition of 2,3-oxidosqualene-lanosterol cyclase (EC 5.4.99.7) (OSC) by new azasqualene derivatives, mimicking the proC-8 and proC-20 carbocationic high-energy intermediates of the cyclization of 2,3-oxidosqualene to lanosterol, was studied using pig liver microsomes, partially purified pr...

The syntheses of nine palladium(II) complexes of type [Pd(phen)(AA)]+ (where AA is an anion of glycine, L-alanine, L-leucine, L-phenylalanine, L-tyrosine, L-tryptophan, L-valine, L-proline, or L-serine) have been achieved. These palladium(II) complexes have been characterized by ultraviolet-visi...

Four new Pd(II) complexes are presented, [Pd(L1)(Cl)]K (1), [Pd(L1)(Cl)]Na (2), [Pd(L2)(Cl)]Na (3) and [Pd(L2)(H2O)] (4), where the ligands are derived from ortho-vanillin and either l-glutamic acid (L1) or l-tyrosine (L2). The complexes were characterized by X-ray diffraction studies, ESI-MS, I...

Seven new palladium(II) complexes (1–7) with 4-toluenesulfonyl-L-amino acid dianion and 2, 2′-biquinoline (bqu)/1,4-diaminobutane (dab) have been synthesized and characterized by elemental analysis, IR, 1H NMR, and mass spectra techniques. Crystal structure of the complex (7) has been determin...

The substitution reactions of the 2,2′-biquinoline (biq) complex cis-[Pd(biq)Cl2] with different amino acids, namely, glycine (glyH), l-serine (serH), l-tyrosine (tyrH), l-phenylalanine (pheH) and l-alanine (alaH) have been investigated. The new complexes [Pd(biq)(gly)]Cl, [Pd(biq)(ser)]PF6·0....

The interaction of the lanthanum(III) La(III)–L (L=N,N′-bis-(1-carboxy-2-methylpropyl)-1,10-phenanthroline-2,9-dimethanamine) complex with calf thymus DNA was studied by electronic spectra, fluorescence spectra and circular dichroic spectra. The La(III)–L complex was assayed for antitumor act...

Two naphthaquinone pigments, 5-deoxyfusarubin and anhydro-5-deoxyfusarubin, were isolated from a yellow strain of the fungus Nectria haematococca. The 13C NMR spectra of 2 biosynthetically labelled from [1-13C]acetate confirmed the structures of the pigments and established the heptaketide origi...

A new 2-aza-anthraquinone 6-O-demethyl-5-deoxybostrycoidin was isolated from cultures of a yellow mutant of the fungusNectria haematococca grown in a medium enriched in asparagine. The results obtained with this family of nitrogen-containing quinones are discussed in relation to our knowledge ab...

The mutagenic activity of 15 different mono-, di-, tri-, and tetramethyl derivatives of the food mutagen IQx (2-amino-3-methylimidazo[4,5-f]quinoxaline), one diphenyl derivative of IQx and two phenyl derivatives of 5-MeIQx (2-amino-3,5-dimethylimidazo[4,5-f]quinoxaline) were studied in the Ames ...

A straightforward method for the synthesis of 5/6-substituted 3-trifluoromethylbenzo[b]thiophenes and their precursor o-fluorinated trifluoro acetophenones is reported.

Learning is accompanied by temporal compression and sharpening of neuronal firing sequences. In this issue of Neuron, Adler et al. (2019), using a motor skill paradigm and its variant, uncover a dual role for somatostatin interneuron regulation to support ensemble compaction and protection in le...

BackgroundSomatostatin analogs are the backbone of neuroendocrine neoplasms treatment. Biliary stone disease is a potentially severe adverse event of somatostatin analogs: an increased incidence has been reported in somatostatin analogs-treated acromegalic patients, but studies on patients with ...

Many cellular processes, including pulsatile release of insulin, are triggered by increase of cytoplasmic Ca2+. This study examines how somatostatin affects glucose generation of cytoplasmic Ca2+ oscillations in mouse islets in absence and presence of tolbutamide blockade of the KATP channels. C...

Neuroendocrine breast cancer (NEBC) is a group of rare tumors, which could benefit from therapy targeting the somatostatin receptors (SSTRs). In particular, SSTR2A and SSTR5 are potential targets given their consistent expression in gastrointestinal and pancreatic primary and metastatic neuroend...